Structure-activity relationship study on N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinehexanamides, a class of 5-HT7 receptor agents. 2.

No abstract is available for this paper.

• Publication year

  2007

• Venue

  Journal of Medicinal Chemistry

• Publication date

  2007-07-25

• Fields of study

  Medicine, Chemistry

• Identifiers
  DOI 10.1021/JM070487NPMID 17649988
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

• Enhancement of the anti-immobility action of antidepressants by a selective 5-HT7 receptor antagonist in the forced swimming test in mice.

  2007cited by this paper
• The involvement of dopamine in the modulation of sleep and waking.

  2007cited by this paper
• Effects of the 5-HT7 receptor antagonist SB-269970 on rat hormonal and temperature responses to the 5-HT1A/7 receptor agonist 8-OH-DPAT.

  2006cited by this paper
• Receptor-based pharmacophores for serotonin 5-HT7R antagonists-implications to selectivity.

  2006cited by this paper
• Potential anxiolytic and antidepressant effects of the selective 5-HT7 receptor antagonist SB 269970 after intrahippocampal administration to rats.

  2006cited by this paper
• An mRNA expression analysis of stimulation and blockade of 5-HT7 receptors during memory consolidation.

  2006cited by this paper
• Genetic knockout and pharmacological blockade studies of the 5-HT7 receptor suggest therapeutic potential in depression.

  2005cited by this paper
• Serotonin 5-HT7 receptors coupled to induction of interleukin-6 in human microglial MC-3 cells.

  2005cited by this paper
• 5-HT7 receptor inhibition and inactivation induce antidepressantlike behavior and sleep pattern.

  2005cited by this paper
• Effects of a 5-HT7 receptor antagonist DR4004 on the exploratory behavior in a novel environment and on brain monoamine dynamics in mice.

  2005cited by this paper
• Contribution of 5-HT2 Receptor Subtypes to Sleep–Wakefulness and Respiratory Control, and Functional Adaptations in Knock-Out Mice Lacking 5-HT2A Receptors

  2005cited by this paper
• Pre‐ and postsynaptic localization of the 5‐HT7 receptor in rat dorsal spinal cord: Immunocytochemical evidence

  2005cited by this paper
• Effects of the 5-HT7 receptor antagonists SB-269970 and DR 4004 in autoshaping Pavlovian/instrumental learning task.

  2004cited by this paper
• Studies on 1‐arylpiperazine derivatives with affinity for rat 5‐HT7 and 5‐HT1A receptors

  2004cited by this paper
• Structure-affinity relationship study on N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinealkylamides, a new class of 5-hydroxytryptamine7 receptor agents.

  2004cited by this paper
• Functional, molecular and pharmacological advances in 5-HT7 receptor research.

  2004cited by this paper
• Synthesis and structure-affinity relationships of 1-[omega-(4-aryl-1-piperazinyl)alkyl]-1-aryl ketones as 5-HT(7) receptor ligands.

  2003cited by this paper
• Characterization of the 5-HT(7) receptor. Determination of the pharmacophore for 5-HT(7) receptor agonism and CoMFA-based modeling of the agonist binding site.

  2003cited by this paper
• 5‐Hydroxytryptamine7 (5‐HT7) receptor immunoreactivity‐positive ‘stigmoid body’‐like structure in developing rat brains

  2003cited by this paper
• Differential modulation of Ih by 5‐HT receptors in mouse CA1 hippocampal neurons

  2002cited by this paper
• Localization of 5-HT(7) receptors in rat brain by immunocytochemistry, in situ hybridization, and agonist stimulated cFos expression.

  2001cited by this paper
• Subcellular distribution of 5‐HT1b and 5‐HT7 receptors in the mouse suprachiasmatic nucleus

  2001cited by this paper
• Reversed-phase high-performance liquid chromatography (RP-HPLC) determination of lipophilicity of furocoumarins: relationship with DNA interaction.

  2001cited by this paper
• D2/D3 Dopamine Receptor Heterodimers Exhibit Unique Functional Properties*

  2001cited by this paper
• Effects of Antidepressants on 5-HT7 Receptor Regulation in the Rat Hypothalamus

  1999cited by this paper
• Cloning, expression and pharmacology of a truncated splice variant of the human 5-HT7 receptor (h5-HT7b).

  1997cited by this paper
• Characterization of a postjunctional 5-HT receptor mediating relaxation of guinea-pig isolated ileum.

  1995cited by this paper
• Activity of aromatic substituted phenylpiperazines lacking affinity for dopamine binding sites in a preclinical test of antipsychotic efficacy.

  1989cited by this paper
• Effector coupling mechanisms of the cloned 5-HT1A receptor.

  1989cited by this paper
• [3H]Ketanserin (R 41 468), a selective 3H-ligand for serotonin2 receptor binding sites. Binding properties, brain distribution, and functional role.

  1982cited by this paper
• Relationship between the inhibition constant (K1) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction.

  1973cited by this paper
• Psychosedative agents. N-(4-phenyl-1-piperazinylalkyl)-substituted cyclic imides.

  1969cited by this paper

• 5-Hydroxytryptamine receptors in GtoPdb v.2025.1

  2025cites this paper
• Novel Dual 5-HT7 Antagonists and Sodium Channel Inhibitors as Potential Therapeutic Agents with Antidepressant and Anxiolytic Activities

  2025influential citation
• Dopamine receptors in GtoPdb v.2025.3

  2025cites this paper
• 5-Hydroxytryptamine receptors in GtoPdb v.2025.3

  2025cites this paper
• Luminescence and In-Silico Studies of Binding Interactions of Arylpiperazinyl-Butyl)Benzoxazolone Synthetic Compounds with Bovine Serum Albumin

  2022cites this paper
• Knowledge-Based Design of Long-Chain Arylpiperazine Derivatives Targeting Multiple Serotonin Receptors as Potential Candidates for Treatment of Autism Spectrum Disorder.

  2021cites this paper
• Synthesis and Biological Evaluation of 99mTc-Labeled Phenylpiperazine Derivatives as Selective Serotonin-7 Receptor Ligands for Brain Tumor Imaging.

  2021cites this paper
• Privileged scaffold-based design to identify a novel drug-like 5-HT7 receptor-preferring agonist to target Fragile X syndrome.

  2020cites this paper
• Rational Design of Multitarget-Directed Ligands: Strategies and Emerging Paradigms.

  2019cites this paper
• 5-HT1D receptors inhibit the monosynaptic stretch reflex by modulating C-fiber activity.

  2019cites this paper
• Structure-activity relationships of serotonin 5-HT7 receptors ligands: A review.

  2019cites this paper
• Synthesis and antidepressant-like activity of novel aralkyl piperazine derivatives targeting SSRI/5-HT1A/5-HT7.

  2018cites this paper
• Pharmacology and Therapeutic Potential of the 5-HT7 Receptor.

  2018cites this paper
• Synthesis and antidepressant activity of a series of arylalkanol and aralkyl piperazine derivatives targeting SSRI/5-HT1A/5-HT7.

  2017cites this paper
• Low-basicity 5-HT7 Receptor Agonists Synthesized Using the van Leusen Multicomponent Protocol

  2017cites this paper
• Involvement of Brain 5-HT 7 Receptors in the Formation of Stress Adaptation in Mice

  2017cites this paper
• An Algorithm to Identify Target-Selective Ligands – A Case Study of 5-HT7/5-HT1A Receptor Selectivity

  2016cites this paper
• Synthesis and biological evaluation of 2-fluoro and 3-trifluoromethyl-phenyl-piperazinylalkyl derivatives of 1H-imidazo[2,1-f]purine-2,4(3H,8H)-dione as potential antidepressant agents

  2016cites this paper
• Structural modifications of the serotonin 5-HT7 receptor agonist N-(4-cyanophenylmethyl)-4-(2-biphenyl)-1-piperazinehexanamide (LP-211) to improve in vitro microsomal stability: A case study.

  2016cites this paper
• Activation of 5-hyrdoxytryptamine 7 receptors within the rat nucleus tractus solitarii modulates synaptic properties.

  2016cites this paper
• How to Choose the Suitable Template for Homology Modelling of GPCRs: 5‐HT7 Receptor as a Test Case

  2016cites this paper
• Targeting the Serotonin 5-HT7 Receptor in the Search for Treatments for CNS Disorders: Rationale and Progress to Date

  2015cites this paper
• The 5-HT7 receptor as a potential target for treating drug and alcohol abuse

  2015influential citation
• Structure-activity relationships and molecular studies of novel arylpiperazinylalkyl purine-2,4-diones and purine-2,4,8-triones with antidepressant and anxiolytic-like activity.

  2015cites this paper
• Towards novel 5-HT7versus 5-HT1A receptor ligands among LCAPs with cyclic amino acid amide fragments: design, synthesis, and antidepressant properties. Part II.

  2015cites this paper
• Rational Design, Pharmacomodulation, and Synthesis of Dual 5-Hydroxytryptamine 7 (5-HT7)/5-Hydroxytryptamine 2A (5-HT2A) Receptor Antagonists and Evaluation by [(18)F]-PET Imaging in a Primate Brain.

  2015cites this paper
• The 5-HT 7 receptor as a potential target for treating drug and alcohol abuse

  2015influential citation
• Receptor Activity 2C and 5-HT 2B Regulated by 5-HT Motoneuron Excitability and Muscle Spasms Are

  2015cites this paper
• Design, synthesis, radiolabeling and in vivo evaluation of potential positron emission tomography (PET) radioligands for brain imaging of the 5-HT₇ receptor.

  2014cites this paper
• Selective agonists for serotonin 7 (5-HT7) receptor and their applications in preclinical models: an overview

  2014cites this paper
• Serotonin modulation of macrophage polarization: inflammation and beyond.

  2014cites this paper
• Synthesis, radiolabeling and in vivo evaluation of [(11)C](R)-1-[4-[2-(4-methoxyphenyl)phenyl]piperazin-1-yl]-3-(2-pyrazinyloxy)-2-propanol, a potential PET radioligand for the 5-HT(7) receptor.

  2014cites this paper
• Structure-activity relationships and molecular modeling studies of novel arylpiperazinylalkyl 2-benzoxazolones and 2-benzothiazolones as 5-HT(7) and 5-HT(1A) receptor ligands.

  2014cites this paper
• Towards the development of 5-HT₇ ligands combining serotonin-like and arylpiperazine moieties.

  2014cites this paper
• Characterization of the discriminative stimulus properties of the atypical antipsychotic amisulpride in C57BL/6 mice

  2014cites this paper
• Novel highly potent serotonin 5-HT7 receptor ligands: structural modifications to improve pharmacokinetic properties.

  2013cites this paper
• Serotonergic modulation of neuronal activity in the nucleus accumbens following repeated methamphetamine administration in rats.

  2013cites this paper
• The arylpiperazine derivatives N-(4-cyanophenylmethyl)-4-(2-diphenyl)-1-piperazinehexanamide and N-benzyl-4-(2-diphenyl)-1-piperazinehexanamide exert a long-lasting inhibition of human serotonin 5-HT7 receptor binding and cAMP signaling

  2013cites this paper
• Towards metabolically stable 5-HT7 receptor ligands: a study on 1-arylpiperazine derivatives and related isosters

  2013cites this paper
• Acute 5-HT7 receptor activation increases NMDA-evoked currents and differentially alters NMDA receptor subunit phosphorylation and trafficking in hippocampal neurons

  2013cites this paper
• The multiobjective based design, synthesis and evaluation of the arylsulfonamide/amide derivatives of aryloxyethyl- and arylthioethyl- piperidines and pyrrolidines as a novel class of potent 5-HT₇ receptor antagonists.

  2012cites this paper
• Investigations on the 1-(2-biphenyl)piperazine motif: identification of new potent and selective ligands for the serotonin(7) (5-HT(7)) receptor with agonist or antagonist action in vitro or ex vivo.

  2012cites this paper
• Activation of 5-HT7 receptors increases neuronal platelet-derived growth factor β receptor expression.

  2012cites this paper
• Secondary mechanical allodynia and hyperalgesia depend on descending facilitation mediated by spinal 5-HT₄, 5-HT₆ and 5-HT₇ receptors.

  2012influential citation
• Assessment of 5-HT7 Receptor Agonists Selectivity Using Nociceptive and Thermoregulation Tests in Knockout versus Wild-Type Mice

  2012cites this paper
• Synthesis and toxicopharmacological evaluation of m-hydroxymexiletine, the first metabolite of mexiletine more potent than the parent compound on voltage-gated sodium channels.

  2012cites this paper
• Polysynaptic excitatory postsynaptic potentials that trigger spasms after spinal cord injury in rats are inhibited by 5-HT1B and 5-HT1F receptors.

  2011cites this paper
• Motoneuron excitability and muscle spasms are regulated by 5-HT2B and 5-HT2C receptor activity.

  2011cites this paper
• Serotonin 5-HT7 receptor agents: Structure-activity relationships and potential therapeutic applications in central nervous system disorders.

  2011cites this paper
• Latest advances towards the discovery of 5-HT(7) receptor ligands.

  2011cites this paper
• Role of peripheral 5‐HT4, 5‐HT6, and 5‐HT7 receptors in development and maintenance of secondary mechanical allodynia and hyperalgesia

  2011cites this paper
• 1F and 5-HT 1B inhibited by 5-HT trigger spasms after spinal cord injury in rats are Polysynaptic excitatory postsynaptic potentials that

  2011cites this paper
• 5-HT7 receptor modulators: a medicinal chemistry survey of recent patent literature (2004 – 2009)

  2010cites this paper
• 5-HT 7 receptor modulators: a medicinal chemistry survey

  2010cites this paper
• Application of desirability-based multi(bi)-objective optimization in the design of selective arylpiperazine derivates for the 5-HT1A serotonin receptor.

  2009cites this paper
• Determination of 1-aryl-4-propylpiperazine pKa values: the substituent on aryl modulates basicity.

  2009cites this paper
• Benzimidazolone-based serotonin 5-HT1A or 5-HT7R ligands: synthesis and biological evaluation.

  2009cites this paper
• Recent Advances on the 5-HT5A, 5-HT6 and 5-HT7 Receptors

  2008cites this paper
• Effect of some P-glycoprotein modulators on Rhodamine-123 absorption in guinea-pig ileum.

  2008cites this paper
• (Phenylpiperazinyl-butyl)oxindoles as selective 5-HT7 receptor antagonists.

  2008cites this paper
• Structural modifications of N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinehexanamides: influence on lipophilicity and 5-HT7 receptor activity. Part III.

  2008cites this paper